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• 产品描述： Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

• 靶点： cdc2/cyclin B:0.65 μM (IC50);cdk2/cyclin A:0.7 μM (IC50);Cdk2/cyclin E2:0.7 μM (IC50);CDK5/p35:0.16 μM (IC50);GST-erk1:30 μM (IC50);erk1:34 μM (IC50);erk2:14 μM (IC50);IR tyrosine kinase:70 μM (IC50);CDK

• 体内研究：
  Compare with normal controls, Seliciclib (Roscovitine) downregulates phosphorylated ERK1/2 and PPARγ with concomitant increase in E-cadherin, but decrease in Vimentin and Collagen IV. Correspondingly, Seliciclib decreases renal tubulointerstitial fibrosis of diabetic rats. Seliciclib (Roscovitine) is effective in decreasing tubulointerstitial fibrosis via the ERK1/2/PPARγ pathway in diabetic rats. Seliciclib (Roscovitine) (16.5 mg/kg) significantly reduces the rate of tumor growth and increases survival of treated mice. Strikingly, Seliciclib (Roscovitine) treatment leads to complete tumor disappearance in one mouse (25%); moreover, no tumor regrowth in this mouse is found 5 months after completion of the treatment. Mouse weights do not differ significantly between mice treated with Seliciclib and control mice, and behavioral differences between the two groups are also negligible. These results suggest that Seliciclib can be used effectively as a selective tumor growth inhibitor in HPV+ head and neck cancer

• 参考文献：
  1. Meijer L, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36. 2. Bai X, et al. CDK5 promotes renal tubulointerstitial fibrosis in diabetic nephropathy via erk1/2/pparγ pathway. Oncotarget. 2016 Apr 27. 3. Gary C, et al. Selective antitumor activity of roscovitine in head and neck cancer. Oncotarget. 2016 May 23.

• 溶解性： DMSO  :  ≥  100  mg/mL  (282.13  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.821 ml	14.106 ml	28.213 ml
  5 mM	0.564 ml	2.821 ml	5.643 ml
  10 mM	0.282 ml	1.411 ml	2.821 ml
  50 mM	0.056 ml	0.282 ml	0.564 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *